Safety, Tolerance, and Pharmacokinetics of Single Rising Oral Doses of BILB 1941 ZW Solution in Healthy Male Subjects, Followed With Bioavailability Comparison of BILB 1941 ZW Tablet and Solution Formulation Administered With or Without Food

Boehringer Ingelheim

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Other: standardized breakfast; Drug: BILB 1941 ZW - tablet; Drug: Placebo; Drug: BILB 1941 ZW - solution; Drug: BILB 1941 ZW - single rising dose part

Study type: Interventional

Funder types: Industry

Identifiers

NCT02256787

1201.1

Details and patient eligibility

About

The objective of the current study was to investigate the safety, tolerability, and pharmacokinetics of BILB 1941 ZW following the administration of single rising doses from 5 mg to 300 mg. In addition the bioavailability of the 60 mg dose given fasted and after a high-fat breakfast was to be be investigated

Enrollment: 56 patients

Sex: Male

Ages: 18 to 50 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

1. Healthy males according to the following criteria based upon a complete medical history, including the physical examination, vital signs (BP, PR), 12-lead ECG, clinical laboratory tests:

   1.1 No finding deviating from normal and of clinical relevance

   1.2 No evidence of a clinically relevant concomitant disease

2. Age ≥18 and Age ≤50 years, BMI ≥18.5 and BMI ≤29.9 kg/m2 (Body Mass Index)

3. Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local legislation

Exclusion criteria

• Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
• History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders, including a clinical history of viral hepatitis, or serological evidence of active Hepatitis B or Hepatitis C infection
• History of orthostatic hypotension, fainting spells and blackouts
• Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
• Chronic or relevant acute infections
• History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
• Intake of drugs with a long half-life (> 24 hours) within 1 month prior to administration
• Use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial
• Participation in another trial with an investigational drug within 1 month prior to administration or during the trial
• Smoker (> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on trial days
• Alcohol abuse (> 60 g/day)
• Drug abuse
• Blood donation of more than 100 mL within 1 month prior to administration or during the trial
• Excessive physical activities within 5 days prior to administration or during the trial
• Any laboratory value outside the clinically accepted reference range and of clinical relevance
• History of any familial bleeding disorder

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Parallel Assignment

Masking: Double Blind

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56 participants in 5 patient groups, including a placebo group

BILB 1941 ZW - single rising dose

Experimental group

Description:

Single rising dose part

Treatment:

Drug: BILB 1941 ZW - single rising dose part

Placebo

Placebo Comparator group

Description:

Single rising dose part

Treatment:

Drug: Placebo

BILB 1941 ZW - tablet - fasted

Experimental group

Description:

Relative bioavailability: The oral solution fasted should be compared with the solid form fasted and after a standardized breakfast

Treatment:

Drug: BILB 1941 ZW - tablet

BILB 1941 ZW - solution

Experimental group

Description:

Relative bioavailability: The oral solution fasted should be compared with the solid form fasted and after a standardized breakfast

Treatment:

Drug: BILB 1941 ZW - solution

BILB 1941 ZW - tablet - fed

Experimental group

Description:

Relative bioavailability: The oral solution fasted should be compared with the solid form fasted and after a standardized breakfast

Treatment:

Drug: BILB 1941 ZW - tablet

Other: standardized breakfast